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Otolaryngologia Polska = the Polish... Dec 2023A novel strategy for the treatment of allergic rhinitis results from the innovative combination of antihistamine and intranasal corticosteroid drugs. By combining two...
A novel strategy for the treatment of allergic rhinitis results from the innovative combination of antihistamine and intranasal corticosteroid drugs. By combining two preparations with different mechanism of action, this novel approach facilitates quick and effective controls of all upper respiratory tract allergy symptoms. The article presents the results of a study of olopatadine hydrochloride and mometasone furoate fixed-dose combination (GSP301) administered intranasally from a spray formulation, with an attempt at positioning the treatment within the ARIA and EPOS guidelines.
Topics: Humans; Mometasone Furoate; Olopatadine Hydrochloride; Administration, Intranasal; Sinusitis; Female; Male; Adult; Anti-Allergic Agents; Drug Combinations; Middle Aged; Treatment Outcome; Rhinitis, Allergic; Rhinitis; Rhinosinusitis
PubMed: 38706259
DOI: 10.5604/01.3001.0054.0941 -
Journal of Ocular Pharmacology and... Mar 2024Topical antihistamines, such as olopatadine hydrochloride, an H1 receptor antagonist, are commonly prescribed for treating allergic conjunctivitis. Drug delivery via...
Topical antihistamines, such as olopatadine hydrochloride, an H1 receptor antagonist, are commonly prescribed for treating allergic conjunctivitis. Drug delivery via eye drops has many deficiencies including a short residence time due to tear drainage via the nasolacrimal duct, which results in a low bioavailability and potential for side effects. These deficiencies could be mitigated by a drug-eluting contact lens such as the recently approved ACUVUE THERAVISION™ WITH KETOTIFEN which is a daily disposable etafilcon, a drug-eluting contact lens with ketotifen (19 μg per lens). Here, we investigate the feasibility of designing a drug-eluting lens with sustained release of olopatadine for treating allergies using an extended wear lens. Nanobarrier depots composed of vitamin-E (VE) are formed through direct entrapment by ethanol-driven swelling. The drug-loaded lenses are characterized for transparency and water content. release is measured under sink conditions and fitted to a diffusion control release model to determine diffusivity and partition coefficient. studies indicate that ACUVUE OASYS and ACUVUE TruEye™ lenses loaded with ∼0.3 g of VE/g of hydrogel effectively prolong olopatadine dynamics by 7-fold and 375-fold, respectively. Incorporation of VE into the lenses retains visible light transmission and other properties. The VE incorporation in commercial lenses significantly increases the release duration offering the possibility of antiallergy extended wear lenses.
Topics: Olopatadine Hydrochloride; Vitamin E; Ketotifen; Contact Lenses; Vitamins
PubMed: 38489059
DOI: 10.1089/jop.2023.0111 -
JAMA Mar 2024Allergic rhinitis affects an estimated 15% of the US population (approximately 50 million individuals) and is associated with the presence of asthma, eczema, chronic or... (Review)
Review
IMPORTANCE
Allergic rhinitis affects an estimated 15% of the US population (approximately 50 million individuals) and is associated with the presence of asthma, eczema, chronic or recurrent sinusitis, cough, and both tension and migraine headaches.
OBSERVATIONS
Allergic rhinitis occurs when disruption of the epithelial barrier allows allergens to penetrate the mucosal epithelium of nasal passages, inducing a T-helper type 2 inflammatory response and production of allergen-specific IgE. Allergic rhinitis typically presents with symptoms of nasal congestion, rhinorrhea, postnasal drainage, sneezing, and itching of the eyes, nose, and throat. In an international study, the most common symptoms of allergic rhinitis were rhinorrhea (90.38%) and nasal congestion (94.23%). Patients with nonallergic rhinitis present primarily with nasal congestion and postnasal drainage frequently associated with sinus pressure, ear plugging, muffled sounds and pain, and eustachian tube dysfunction that is less responsive to nasal corticosteroids. Patients with seasonal allergic rhinitis typically have physical examination findings of edematous and pale turbinates. Patients with perennial allergic rhinitis typically have erythematous and inflamed turbinates with serous secretions that appear similar to other forms of chronic rhinitis at physical examination. Patients with nonallergic rhinitis have negative test results for specific IgE aeroallergens. Intermittent allergic rhinitis is defined as symptoms occurring less than 4 consecutive days/week or less than 4 consecutive weeks/year. Persistent allergic rhinitis is defined as symptoms occurring more often than 4 consecutive days/week and for more than 4 consecutive weeks/year. Patients with allergic rhinitis should avoid inciting allergens. In addition, first-line treatment for mild intermittent or mild persistent allergic rhinitis may include a second-generation H1 antihistamine (eg, cetirizine, fexofenadine, desloratadine, loratadine) or an intranasal antihistamine (eg, azelastine, olopatadine), whereas patients with persistent moderate to severe allergic rhinitis should be treated initially with an intranasal corticosteroid (eg, fluticasone, triamcinolone, budesonide, mometasone) either alone or in combination with an intranasal antihistamine. In contrast, first-line therapy for patients with nonallergic rhinitis consists of an intranasal antihistamine as monotherapy or in combination with an intranasal corticosteroid.
CONCLUSIONS AND RELEVANCE
Allergic rhinitis is associated with symptoms of nasal congestion, sneezing, and itching of the eyes, nose, and throat. Patients with allergic rhinitis should be instructed to avoid inciting allergens. Therapies include second-generation H1 antihistamines (eg, cetirizine, fexofenadine, desloratadine, loratadine), intranasal antihistamines (eg, azelastine, olopatadine), and intranasal corticosteroids (eg, fluticasone, triamcinolone, budesonide, mometasone) and should be selected based on the severity and frequency of symptoms and patient preference.
Topics: Humans; Budesonide; Cetirizine; Fluticasone; Histamine H1 Antagonists; Immunoglobulin E; Mometasone Furoate; Olopatadine Hydrochloride; Pruritus; Rhinitis, Allergic; Rhinorrhea; Sneezing; Triamcinolone; Glucocorticoids; Rhinitis; Histamine Antagonists; Administration, Intranasal
PubMed: 38470381
DOI: 10.1001/jama.2024.0530 -
BMC Chemistry Feb 2024Four sensitive and fast analytical approaches relied on ion pairing with eosin Y were built up and evaluated using spectroscopy for determination of Alcaftadine and...
Determination of antihistaminic drugs alcaftadine and olopatadine hydrochloride via ion-pairing with eosin Y as a spectrofluorimetric and spectrophotometric probe: application to dosage forms.
Four sensitive and fast analytical approaches relied on ion pairing with eosin Y were built up and evaluated using spectroscopy for determination of Alcaftadine and Olopatadine hydrochloride with high sensitivity and selectivity. Two spectrofluorimetric techniques were employed to observe the quenching effect of Alcaftadine or Olopatadine hydrochloride on the intrinsic fluorescence of eosin Y in a 0.1 M acetate buffer solution at pH 3.8 and 3.3 for Alcaftadine and Olopatadine hydrochloride, respectively. Those methods are considered the first spectrofluorimetric methods for Alcaftadine and Olopatadine hydrochloride assay. The fluorescence quenching effect was linear with concentration ranging from 150 to 2000 and 200 to 2000 ng mL for Alcaftadine and Olopatadine hydrochloride, respectively. In the two spectrophotometric techniques, the absorbance of the produced ion-pair was monitored at 548 and 547 nm in aqueous buffered solution at pH 3.8 and 3.3 for Alcaftadine and Olopatadine hydrochloride, respectively. Beer's law was obeyed in the concentrations range of 0.8-8.0 and 1.0-10.0 µg mL. The four techniques were evaluated in accordance with ICH requirements and were effectively used to analyze dosage forms with a high percent recovery.
PubMed: 38388420
DOI: 10.1186/s13065-024-01137-y -
Veterinary Ophthalmology Dec 2023The objective of the study was to evaluate the efficacy of a once a day, over the counter antihistamine eye drop, 0.7% olopatadine hydrochloride, in treating or...
OBJECTIVE
The objective of the study was to evaluate the efficacy of a once a day, over the counter antihistamine eye drop, 0.7% olopatadine hydrochloride, in treating or preventing experimentally induced allergic conjunctivitis in dogs.
ANIMALS STUDIED
Twelve systemically healthy pet dogs with no known history of allergies or atopic dermatitis, and in the past 12 months had no known ocular abnormalities.
PROCEDURES
Dogs were randomly assigned to two groups: "Treatment" which received topical 0.7% olopatadine hydrochloride and "Control" which received artificial tears. Dogs received the antihistamine eye drops before (Phase 1) or after (Phase 2) receiving a compounded ophthalmic histamine solution to induce clinical signs of allergic conjunctivitis. Conjunctival hyperemia, chemosis, follicles, ocular discharge, and ocular pruritus were graded, and photographs were used to document changes. Schirmer tear test values, fluorescein staining, and intraocular pressures were monitored throughout.
RESULTS
In both Phase 1 and Phase 2, conjunctival scores increased 10 min after histamine administration (p < .05). There was no difference between maximum overall conjunctival scores between treatment and control groups in either phase or when comparing treatment groups of Phase 1 to Phase 2 (p > .05). However, treatment groups in Phase 2 did have a higher maximum conjunctival chemosis score and spent more time at their maximum chemosis score when compared to Phase 1 (p < .05).
CONCLUSION
Olopatadine may be beneficial as prophylaxis to reduce the degree and duration of clinical signs of allergic conjunctivitis.
PubMed: 38066706
DOI: 10.1111/vop.13168 -
Clinical Ophthalmology (Auckland, N.Z.) 2023To study the efficacy and toxic effects of bepotastine besilate 1.5% preservative-free (BB-PF) and olopatadine 0.2% BAK-preserved (OL-BAK) drops on the ocular surface of... (Clinical Trial)
Clinical Trial
Efficacy and Toxicity Evaluation of Bepotastine Besilate 1.5% Preservative-Free Eye Drops Vs Olopatadine Hydrochloride 0.2% Bak-Preserved Eye Drops in Patients with Allergic Conjunctivitis.
PURPOSE
To study the efficacy and toxic effects of bepotastine besilate 1.5% preservative-free (BB-PF) and olopatadine 0.2% BAK-preserved (OL-BAK) drops on the ocular surface of patients with allergic conjunctivitis.
PATIENTS AND METHODS
Ninety-seven patients with allergic conjunctivitis diagnosis participated in a prospective, multicenter, randomized, double-blind, controlled, parallel-group clinical trial. Patients received either BB-PF (n=48) or OL-BAK (n=49), both administered once daily in the morning. The patients were followed for 60 days. Ocular itching was the primary outcome measure. Secondary outcomes included ocular symptoms, signs, and non-ocular symptoms associated with rhinoconjunctivitis. Conjunctival impression cytology (CIC) was performed to evaluate histopathological changes related to the toxic effects of preservatives.
RESULTS
BB-PF treatment was associated with a 1.30 more probability of diminished ocular itching than OL-BAK (odds ratio (OR)=1.30; 95% CI=(0.96-1.7); p=0.086). No statistically significant differences were found between treatments in the resolution of other ocular symptoms or signs, except for tearing, which was superior in the BB-PF (OR=1.37; 95% (1.26-1.47); p<0.0001). BB-PF was superior in terms of the resolution of rhinorrhea (p=0.040) and nasal itching (p=0.037). After 60 days of treatment, the BB-PF group exhibited 2.0 times higher probability of having a lower Nelson scale score compared to the OL-BAK group (OR=2.00; 95% CI=(1.19-3.34); p=0.010).
CONCLUSION
Both medications presented a similar efficacy in terms of the resolution of ocular signs and symptoms associated with ocular conjunctivitis. BB-PF is superior in the resolution of non-ocular symptoms and safer for the ocular surface than OL-BAK.
PubMed: 38026598
DOI: 10.2147/OPTH.S431889 -
Eye (London, England) Apr 2024To explore the efficacy and relevant mechanism of 0.05% cyclosporine A (CsA) eye drops (II) monotherapy in patients with allergic conjunctivitis-associated dry eye... (Randomized Controlled Trial)
Randomized Controlled Trial
PURPOSE
To explore the efficacy and relevant mechanism of 0.05% cyclosporine A (CsA) eye drops (II) monotherapy in patients with allergic conjunctivitis-associated dry eye (ACDE).
METHODS
Prospective, randomized, controlled study. Fifty-three patients with mild-to-moderate ACDE were randomly assigned to two groups. The CsA group received 0.05% CsA eye drops (II) monotherapy four times daily. The control group received 0.1% olopatadine twice daily combined with 0.1% preservative-free artificial tears four times daily. Clinical symptoms and signs, tear total IgE, and lymphotoxin-α (LT-α) concentrations were assessed at pre- and post-treatment days 7, 30, and 60. And we further measured six tear cytokines levels using a microsphere-based immunoassay.
RESULTS
The CsA group showed significant improvement in symptoms (Ocular Surface Disease Index and itching scores) and signs (conjunctival hyperaemia, conjunctival oedema, conjunctival papillae, tear break-up time (TBUT), corneal fluorescein staining, and goblet cell density) at each follow-up period compared to pre-treatment (all P < 0.050). And its improvement in itching scores (P < 0.001, P = 0.039, and P = 0.031) and TBUT (P = 0.009, P = 0.003, and P = 0.005) was more significant than the control group at all follow-up periods. The tear total IgE, interleukin (IL)-5, IL-6, periostin, eotaxin-3, and MMP-9 levels significantly decreased in the CsA group at day 60 after treatment (all P < 0.050). And the changed values in tear total IgE were positively correlated with the change in itching scores.
CONCLUSIONS
0.05% CsA eye drops (II) monotherapy can rapidly improve the symptoms and signs, especially in ocular itching and TBUT, in patients with ACDE. And its efficacy is superior to 0.1% olopatadine combined with artificial tears. Moreover, CsA downregulates the expression levels of tear inflammatory cytokines, including tear total IgE, IL-5, IL-6, periostin, eotaxin-3, and MMP-9. Among that, the reduction in tear total IgE levels may reflect the improvement of ocular itching.
Topics: Humans; Conjunctivitis, Allergic; Cyclosporine; Ophthalmic Solutions; Olopatadine Hydrochloride; Chemokine CCL26; Matrix Metalloproteinase 9; Lubricant Eye Drops; Interleukin-6; Prospective Studies; Dry Eye Syndromes; Cytokines; Pruritus; Immunoglobulin E; Tears
PubMed: 37904000
DOI: 10.1038/s41433-023-02807-2 -
Scientific Reports Oct 2023Ophthalmic preparations that contain ketorolac tromethamine (KET) and olopatadine HCl (OLO) are used to relieve seasonal allergies and allergic conjunctivitis....
UV spectrophotometric methods for simultaneous determination of ketorolac tromethamine and olopatadine hydrochloride: Application of multiple standard addition for assay of ophthalmic solution.
Ophthalmic preparations that contain ketorolac tromethamine (KET) and olopatadine HCl (OLO) are used to relieve seasonal allergies and allergic conjunctivitis. Simultaneous quantification of KET and OLO was held by validated and simple spectrophotometric methods. KET was determined directly from the fundamental UV absorption spectra (at 323 nm), while OLO was determined after performing either dual wavelength or ratio derivative methods. The first method was based on measuring the absorbance difference (ΔA) between 243 and 291 nm, while the second depended on generating first derivative ratio spectra using 3.0 µg/mL KET as a divisor and measuring OLO responses at 234 nm (minima). Multiple standard addition method was applied to enable the determination of OLO which is considered as the weakly absorbing species as well as the minor component in a challenging dosage form ratio (4:1). The linearity ranges of the developed methods were 3-12 μg/mL and 4-40 μg/mL for KET and OLO, respectively. Simultaneous determination of both drugs was successfully implemented to lab prepared eye drops that contain KET, OLO and benzalkonium chloride as an inactive ingredient. Greenness assessment indicates minimal impact on environment. The developed methods determined the cited drugs with % recovery ± SD of 99.63 ± 0.01 for KET, 100.90 ± 0.02 and 100.31 ± 0.01 for OLO using dual wavelength and first derivative ratio methods, respectively. Using F-test and t-test at confidence level %95 to compare between the results of the presented methods and a reported method show no significant difference which allows precise, accurate, rapid, and simple quantification of quality control samples that contain KET and OLO.
Topics: Humans; Olopatadine Hydrochloride; Ketorolac Tromethamine; Ophthalmic Solutions; Conjunctivitis, Allergic; Spectrophotometry
PubMed: 37875539
DOI: 10.1038/s41598-023-45378-8 -
Inflammopharmacology Feb 2024Morbidity and mortality rates associated with acute lung injury/acute respiratory distress syndrome (ALI/ARDS) are high (30-40%). Nuclear factor-kappa B (NF-κB) is a...
BACKGROUND
Morbidity and mortality rates associated with acute lung injury/acute respiratory distress syndrome (ALI/ARDS) are high (30-40%). Nuclear factor-kappa B (NF-κB) is a transcription factor, associated with transcription of numerous cytokines leading to cytokine storm, and thereby, plays a major role in ALI/ARDS and in advanced COVID-19 syndrome.
METHODS
Considering the role of NF-κB in ALI, cost-effective in silico approaches were utilized in the study to identify potential NF-κB inhibitor based on the docking and pharmacokinetic results. The identified compound was then pharmacologically validated in lipopolysaccharide (LPS) rodent model of acute lung injury. LPS induces ALI by altering alveolar membrane permeability, recruiting activated neutrophils and macrophages to the lungs, and compromising the alveolar membrane integrity and ultimately impairs the gaseous exchange. Furthermore, LPS exposure is associated with exaggerated production of various proinflammatory cytokines in lungs.
RESULTS
Based on in silico studies Olopatadine Hydrochloride (Olo), an FDA-approved drug was found as a potential NF-κB inhibitor which has been reported for the first time, and considered further for the pharmacological validation. Intraperitoneal LPS administration resulted in ALI/ARDS by fulfilling 3 out of the 4 criteria described by ATS committee (2011) published workshop report. However, treatment with Olo attenuated LPS-induced elevation of proinflammatory markers (IL-6 and NF-κB), oxidative stress, neutrophil infiltration, edema, and damage in lungs. Histopathological studies also revealed that Olo treatment significantly ameliorated LPS-induced lung injury, thus conferring improvement in survival. Especially, the effects produced by Olo medium dose (1 mg/kg) were comparable to dexamethasone standard.
CONCLUSION
In nutshell, inhibition of NF-κB pathway by Olo resulted in protection and reduced mortality in LPS- induced ALI and thus has potential to be used clinically to arrest disease progression in ALI/ARDS, since the drug is already in the market. However, the findings warrant further extensive studies, and also future studies can be planned to elucidate its role in COVID-19-associated ARDS or cytokine storm.
Topics: Humans; NF-kappa B; Lipopolysaccharides; Olopatadine Hydrochloride; Cytokine Release Syndrome; Signal Transduction; Acute Lung Injury; I-kappa B Proteins; Respiratory Distress Syndrome; COVID-19; Cytokines
PubMed: 37847473
DOI: 10.1007/s10787-023-01353-3 -
Indian Journal of Ophthalmology May 2023The main objective of this study is to explore the efficacy of olopatadine 0.1% treatment in the resolution of symptoms of vernal keratoconjunctivitis (VKC) among the...
Assessment of the efficacy of olopatadine 0.1% in the treatment of vernal keratoconjunctivitis in terms of clinical improvement based on total ocular symptom score and ocular surface disease index.
PURPOSE
The main objective of this study is to explore the efficacy of olopatadine 0.1% treatment in the resolution of symptoms of vernal keratoconjunctivitis (VKC) among the Indian population.
METHODS
This single-center, prospective cohort study involved 234 patients with VKC. Patients were treated with olopatadine 0.1%, twice daily for a period of 12 weeks and then followed up in 1 week, 4 week, 3 month, and 6 month. The extent of relief in the symptoms of VKC was measured using total ocular symptom score (TOSS) and ocular surface disease index (OSDI).
RESULTS
In the present study, the dropout rate was 5.6%. Total of 136 males and 85 females with a mean age of 37.68 ± 11.35 years completed the study. TOSS score reduced from 58.85 to 5.06 and the OSDI score reduced from 75.41 to 11.2 with statistical significance (P < 0.01) from 1 week to 6 week after olopatadine 0.1% treatment. The data showed relief in subjective symptoms of itching, tearing, and redness, and relief in discomfort in functions related to ocular grittiness, visuals like reading, and environmental like tolerability in dry conditions. Further, olopatadine 0.1% was effective in both males and females, and patients across ages 18-70 years.
CONCLUSION
Based on TOSS and OSDI scores, the findings of this study validate safety and tolerability as revealed by low adverse effects and moderate efficacy of olopatadine 0.1% in reducing VKC symptoms in a broader age group (18-70 years) of both genders.
Topics: Humans; Female; Male; Adult; Middle Aged; Adolescent; Young Adult; Aged; Olopatadine Hydrochloride; Conjunctivitis, Allergic; Prospective Studies; Dibenzoxepins; Eye; Ophthalmic Solutions
PubMed: 37203036
DOI: 10.4103/ijo.IJO_2048_22